Differential effects of flurbiprofen and aspirin on acetazolamide disposition in humans.

Sweeney, Kevin; Chapron, Dennis J.; Antal, Edward J.; Kramer, Paul A.

doi:10.1111/j.1365-2125.1989.tb03451.x

Cited by 14 publications

(6 citation statements)

References 8 publications

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“…Aspirin also displaces acetazolamide from plasma proteins and so raises the effective free drug concentration [108,109]. If a nonsteroidal anti-inflammatory drug needs to be taken with acetazolamide, then flurbiprofen is a safer alternative [110].…”

Section: Interactions With Other Drugsmentioning

confidence: 99%

Safety of carbonic anhydrase inhibitors

Swenson¹

2014

Expert Opinion on Drug Safety

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Common side effects of paresthesias, dyspepsia, lassitude and fatigue in 30 - 40% of patients are generally tolerable or abate, but if not can be partially relieved by bicarbonate supplementation. The most important safety concerns are severe acidosis, respiratory failure and encephalopathy in patients with renal, pulmonary and hepatic disease where caution is critical, as is also the case in persons with sulfa drug allergies.

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Section: Interactions With Other Drugsmentioning

confidence: 99%

Safety of carbonic anhydrase inhibitors

Swenson¹

2014

Expert Opinion on Drug Safety

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“…This is in sharp contrast to ACZ, the most commonly used CAI. ACZ is nearly 100% eliminated by the kidney, where it undergoes extensive tubular secretion [3]. At present, it is not known whether MTZ is secreted by the kidney.…”

Section: Resultsmentioning

confidence: 99%

“…MTZ is a methylated tautomer of acetazolamide (ACZ), the most commonly prescribed CAI. ACZ is eliminated primarily unchanged by the kidneys and is approximately 90% bound to plasma proteins [2,3]. ACZ has been shown to accumulate and cause serious metabolic acidosis in elderly patients and patients with renal insufficiency, including those undergoing haemodialysis and peritoneal dialysis [4 -10].…”

Section: Introductionmentioning

confidence: 99%

Blood disposition and urinary excretion kinetics of methazolamide following oral administration to human subjects

Taft

Nordt

Iyer

et al. 1998

Biopharm. Drug Dispos.

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“…In this study RBC concentrations were only 17 µM at Cmax, and so the absence of observed side-effects is not surprising. Aspirin at very high doses (3.5–5g /day) has been reported to reduce the clearance of therapeutic doses of ACZ by two fold, due to competition at renal transporters 24 . However, given that the rate of microdose elimination appears to be controlled by CA depot-release rather than renal transport rates, an ACZ marker would not be expected to be as greatly affected by high aspirin doses as with a therapeutic dose.…”

Section: Discussionmentioning

confidence: 99%

A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials

Hampson

Babalonis

Lofwall³

et al. 2016

J Clin Psychopharmacol

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Rationale Accurate assessment of medication adherence is critical for determination of medication efficacy in clinical trials, but most current methods have significant limitations. This study tests a sub-therapeutic (microdose) of acetazolamide as a medication ingestion marker, because acetazolamide is rapidly absorbed and excreted without metabolism in urine and can be non-invasively sampled. Methods In a double-blind, placebo-controlled, residential study, ten volunteers received 15 mg oral acetazolamide for four consecutive days. Acetazolamide pharmacokinetics were assessed on Day 3, and its pharmacokinetic and pharmacodynamic interactions with a model medication (30 mg oxycodone) were examined on Day 4. The rate of acetazolamide elimination into urine was followed for several days after dosing cessation. Results Erythrocyte sequestration (half-life= 50.2±18.5h, mean±SD, n=6), resulted in the acetazolamide microdose exhibiting a substantially longer plasma half-life (24.5±5.6 h, n=10) than previously reported for therapeutic doses (3–6 h). Following cessation of dosing, the rate of urinary elimination decreased significantly (F(3,23)=247: p<0.05, n=6) in a predictable manner with low inter-subject variability and a half-life of 16.1±3.8h (n=10). For each of four consecutive mornings after dosing cessation, the rates of urinary acetazolamide elimination remained quantifiable. There was no overall effect of acetazolamide on the pharmacodynamics, Cmax, Tmax or elimination half-life of the model medication tested. Acetazolamide may have modestly increased overall oxycodone exposure (20%, p<0.05) compared with one of the two days when oxycodone was given alone, but there were no observed effects of acetazolamide on oxycodone pharmacodynamic responses. Conclusions Co-formulation of a once-daily trial medication with an acetazolamide microdose may allow estimation of the last time of medication consumption for up to 96h post-dose. Inclusion of acetazolamide may, therefore, provide an inexpensive new method to improve estimates of medication adherence in clinical trials.

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Differential effects of flurbiprofen and aspirin on acetazolamide disposition in humans.

Cited by 14 publications

References 8 publications

Safety of carbonic anhydrase inhibitors

Safety of carbonic anhydrase inhibitors

Blood disposition and urinary excretion kinetics of methazolamide following oral administration to human subjects

A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials

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